Synthesis and Evaluation of Terbenzimidazoles as Topoisomerase I Inhibitors

Qun Sun; Barbara Gatto; Chiang Yu; Angela Liu; Leroy F. Liu; Edmond J. LaVoie

doi:10.1021/jm00018a024

Synthesis and Evaluation of Terbenzimidazoles as Topoisomerase I Inhibitors

Qun Sun, Barbara Gatto, Chiang Yu, Angela Liu, Leroy F. Liu, Edmond J. LaVoie

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79 Citations (Scopus)

Abstract

The synthesis and pharmacological activity of a series of terbenzimidazoles are described. The ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity in RPMI 8402 cells and the camptothecin-resistant CPT-K5 cells. In addition the potential for these compounds to serve as substrates for MDR1 was also determined. Several terbenzimidazoles exhibited similar cytotoxicity against variants of human tumor cells that either overexpress MDR1 or are camptothecin-resistant.

Original language	English
Pages (from-to)	3638-3644
Number of pages	7
Journal	Journal of Medicinal Chemistry
Volume	38
Issue number	18
DOIs	https://doi.org/10.1021/jm00018a024
Publication status	Published - Sept 1 1995
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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title = "Synthesis and Evaluation of Terbenzimidazoles as Topoisomerase I Inhibitors",

abstract = "The synthesis and pharmacological activity of a series of terbenzimidazoles are described. The ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity in RPMI 8402 cells and the camptothecin-resistant CPT-K5 cells. In addition the potential for these compounds to serve as substrates for MDR1 was also determined. Several terbenzimidazoles exhibited similar cytotoxicity against variants of human tumor cells that either overexpress MDR1 or are camptothecin-resistant.",

author = "Qun Sun and Barbara Gatto and Chiang Yu and Angela Liu and Liu, {Leroy F.} and LaVoie, {Edmond J.}",

year = "1995",

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doi = "10.1021/jm00018a024",

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T1 - Synthesis and Evaluation of Terbenzimidazoles as Topoisomerase I Inhibitors

AU - Sun, Qun

AU - Gatto, Barbara

AU - Yu, Chiang

AU - Liu, Angela

AU - Liu, Leroy F.

AU - LaVoie, Edmond J.

PY - 1995/9/1

Y1 - 1995/9/1

N2 - The synthesis and pharmacological activity of a series of terbenzimidazoles are described. The ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity in RPMI 8402 cells and the camptothecin-resistant CPT-K5 cells. In addition the potential for these compounds to serve as substrates for MDR1 was also determined. Several terbenzimidazoles exhibited similar cytotoxicity against variants of human tumor cells that either overexpress MDR1 or are camptothecin-resistant.

AB - The synthesis and pharmacological activity of a series of terbenzimidazoles are described. The ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity in RPMI 8402 cells and the camptothecin-resistant CPT-K5 cells. In addition the potential for these compounds to serve as substrates for MDR1 was also determined. Several terbenzimidazoles exhibited similar cytotoxicity against variants of human tumor cells that either overexpress MDR1 or are camptothecin-resistant.

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JO - Journal of Medicinal Chemistry

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ER -

Synthesis and Evaluation of Terbenzimidazoles as Topoisomerase I Inhibitors

Abstract

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